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1. 发明公开

EP1599183A2 METHOD OF DRUG LOADING IN LIPOSOMES BY GRADIENT 审中-公开
标题翻译：脂质体的方法为药物的费用梯度。
公开(公告)号：EP1599183A2
公开(公告)日：2005-11-30
申请号：EP03787169.6
申请日：2003-11-26
申请人： GILEAD SCIENCES, INC. , Jensen, Gerard M.
发明人： HU, Ning , JENSEN, Gerard, M. , SULIVAN, Michele , YANG, Stephanie
IPC分类号： A61K9/00
CPC分类号： A61K9/127 , A61K9/1277 , A61K9/1278 , A61K31/137 , A61K31/55 , A61K31/704
摘要： A method for encapsulation of pharmaceutical agents (e.g., antineoplastic agents) in liposomes is provided, having preferably a high drug:lipid ratio. Liposomes can be made by a process that loads the drug by an active mechanism using a transmembrane pH gradient. Using this technique, trapping efficiencies approach 100%. Drug:lipid ratios employed are higher than for older traditional liposome preparations, and the release rate of the drug from the liposomes is reduced. After loading, residual acid is quenched with a quenching agent that is base permeable at low temperatures. The residual aciditiy is thus reduced and chemical stability (e.g. against hydrolysis) is enhanced. The stability of both the liposome and the pharmaceutical agent is thus maintained, prior to administration. The pH gradient is, however, present when the liposome is administered in vivo because the quenching agent rapidly exits the liposome.

2. 发明申请

WO2006031857A2 DELIVERING IRON TO AN ANIMAL 审中-公开
标题翻译：将铁交给动物
公开(公告)号：WO2006031857A2
公开(公告)日：2006-03-23
申请号：PCT/US2005/032674
申请日：2005-09-13
申请人： GILEAD SCIENCES, INC. , HU, Ning , JENSEN, Gerard M. , SKENES, Craig , YANG, Stephanie
发明人： HU, Ning , JENSEN, Gerard M. , SKENES, Craig , YANG, Stephanie
IPC分类号： A61K9/127
CPC分类号： A61K33/26 , A61K9/0019 , A61K9/127 , A61K31/285
摘要： The invention provides a method for delivery iron to an animal. This invention further provides a method for treating iron deficiency in an animal.
摘要翻译：本发明提供了将铁输送到动物的方法。本发明还提供了一种治疗动物缺铁的方法。

3. 发明申请

WO2004047801A2 METHOD OF DRUG LOADING IN LIPOSOMES BY GRADIENT 审中-公开
标题翻译：梯度药物在脂质体中的加载方法
公开(公告)号：WO2004047801A2
公开(公告)日：2004-06-10
申请号：PCT/US2003/037964
申请日：2003-11-26
申请人： GILEAD SCIENCES, INC. , JENSEN, Gerard, M. , SULIVAN, Michele , YANG, Stephanie , HU, Ning
发明人： JENSEN, Gerard, M. , SULIVAN, Michele , YANG, Stephanie , HU, Ning
IPC分类号： A61K9/00
CPC分类号： A61K9/127 , A61K9/1277 , A61K9/1278 , A61K31/137 , A61K31/55 , A61K31/704
摘要： A method for encapsulation of pharmaceutical agents (e.g., antineoplastic agents) in liposomes is provided, having preferably a high drug:lipid ratio. Liposomes can be made by a process that loads the drug by an active mechanism using a transmembrane pH gradient. Using this technique, trapping efficiencies approach 100%. Drug:lipid ratios employed are higher than for older traditional liposome preparations, and the release rate of the drug from the liposomes is reduced. After loading, residual acid is quenched with a quenching agent that is base permeable at low temperatures. The residual aciditiy is thus reduced and chemical stability (e.g. against hydrolysis) is enhanced. The stability of both the liposome and the pharmaceutical agent is thus maintained, prior to administration. The pH gradient is, however, present when the liposome is administered in vivo because the quenching agent rapidly exits the liposome.
摘要翻译：提供了用于将药剂（例如抗肿瘤剂）包封在脂质体中的方法，其优选具有高药物：脂质比率。脂质体可以通过使用跨膜pH梯度通过活性机制加载药物的过程来制备。使用这种技术，捕获效率接近100％。所使用的药物：脂质比率高于较老的传统脂质体制剂，并且药物从脂质体的释放速率降低。上样后，残余的酸用低温下碱可渗透的淬火剂淬灭。残留的酸性因此降低并且化学稳定性（例如抗水解）增强。在施用之前，脂质体和药剂的稳定性因此得以保持。然而，当脂质体在体内给药时存在pH梯度，因为猝灭剂迅速离开脂质体。

4. 发明申请

WO2004047800A3 METHOD OF DRUG LOADING IN LIPOSOMES BY GRADIENT 审中-公开
公开(公告)号：WO2004047800A3
公开(公告)日：2004-06-10
申请号：PCT/US2003/037790
申请日：2003-11-26
申请人： GILEAD SCIENCES, INC. , SULIVAN, Michele , YANG, Stephanie , HU, Ning , JENSEN, Gerard, M.
发明人： SULIVAN, Michele , YANG, Stephanie , HU, Ning , JENSEN, Gerard, M.
IPC分类号： A61K9/127
摘要： A method for encapsulation of pharmaceutical agents (e.g., antineoplastic agents) in liposomes is provided, having preferably a high drug:lipid ratio. Liposomes can be made by a process that loads the drug by an active mechanism using a transmembrane pH gradient. Using this technique, trapping efficiencies approach 100%. Drug:lipid ratios employed are higher than for older traditional liposome preparations, and the release rate of the drug from the liposomes is reduced. After loading, residual acid is quenched with a quenching agent that is base permeable at low temperatures. The residual aciditiy is thus reduced and chemical stability (e.g. against hydrolysis) is enhanced. The stability of both the liposome and the pharmaceutical agent is thus maintained, prior to administration. The pH gradient is, however, present when the liposome is administered in vivo because the quenching agent rapidly exits the liposome.

5. 发明申请

WO2005070465A2 LIPID-BASED DISPERSIONS USEFUL FOR DRUG DELIVERY 审中-公开
标题翻译：用于药物递送的基于脂质的分散剂
公开(公告)号：WO2005070465A2
公开(公告)日：2005-08-04
申请号：PCT/US2005/001149
申请日：2005-01-14
申请人： GILEAD SCIENCES, INC. , HU, Ning , JENSEN, Gerard M. , YANG, Stephanie , SU-MING, Chiang
发明人： HU, Ning , JENSEN, Gerard M. , YANG, Stephanie , SU-MING, Chiang
IPC分类号： A61K47/00
CPC分类号： A61K9/127 , A61K9/0019
摘要： The invention provides lipid-based dispersion comprising comprising, a) phosphatidyl choline; b) an anionic phospholipid; optionally c) up to 1% cholesterol by weight of total lipids; and optionally d) a therapeutic agent; wherein the mean particle size measured by dynamic light scattering is less than 100 nm. The invention also provides pharmaceutical compositions comprising such a dispersion as well as methods of producing a therapeutic effect in a mammal comprising administering an effective amount of such a dispersion.
摘要翻译：本发明提供基于脂质的分散体，其包含：a）磷脂酰胆碱; b）阴离子磷脂; 任选地c）总脂质重量高达1％的胆固醇; 和任选地d）治疗剂; 其中通过动态光散射测量的平均粒度小于100nm。本发明还提供包含这种分散体的药物组合物以及在哺乳动物中产生治疗效果的方法，包括施用有效量的这种分散体。

6. 发明申请

WO2022251318A1 PHOSPHOLIPID FORMULATIONS OF 1'-CYANO SUBSTITUTED CARBA-NUCLEOSIDE ANALOGS 审中-公开
公开(公告)号：WO2022251318A1
公开(公告)日：2022-12-01
申请号：PCT/US2022/030866
申请日：2022-05-25
申请人： GILEAD SCIENCES, INC.
发明人： JENSEN, Gerard , KIM, Youngri , LEE, Kian Yong , PHAM, Huy , UPTON, Thomas , YANG, Stephanie
IPC分类号： A61K9/127 , A61K31/706 , A61K9/19 , A61K47/12 , A61K47/26 , A61K9/00 , A61K31/00
摘要： The disclosure provides pharmaceutical formulations of the compound of Formula (I) : Formula (I) or a pharmaceutically acceptable salt thereof.

7. 发明公开

EP1706148A2 LIPID-BASED DISPERSIONS USEFUL FOR DRUG DELIVERY 审中-公开
标题翻译：分散体脂质基于内容的有效管理
公开(公告)号：EP1706148A2
公开(公告)日：2006-10-04
申请号：EP05705671.5
申请日：2005-01-14
申请人： GILEAD SCIENCES, INC.
发明人： HU, Ning , JENSEN, Gerard M. , YANG, Stephanie , SU-MING, Chiang
IPC分类号： A61K47/00
CPC分类号： A61K9/127 , A61K9/0019
摘要： The invention provides lipid-based dispersion comprising comprising, a) phosphatidyl choline; b) an anionic phospholipid; optionally c) up to 1% cholesterol by weight of total lipids; and optionally d) a therapeutic agent; wherein the mean particle size measured by dynamic light scattering is less than 100 nm. The invention also provides pharmaceutical compositions comprising such a dispersion as well as methods of producing a therapeutic effect in a mammal comprising administering an effective amount of such a dispersion.

8. 发明公开

EP4346772A1 PHOSPHOLIPID FORMULATIONS OF 1'-CYANO SUBSTITUTED CARBA-NUCLEOSIDE ANALOGS 审中-实审
公开(公告)号：EP4346772A1
公开(公告)日：2024-04-10
申请号：EP22735692.0
申请日：2022-05-25
申请人： GILEAD SCIENCES, INC.
发明人： JENSEN, Gerard , KIM, Youngri , LEE, Kian Yong , PHAM, Huy , UPTON, Thomas , YANG, Stephanie
IPC分类号： A61K9/127 , A61K31/706 , A61K9/19 , A61K47/12 , A61K47/26 , A61K9/00 , A61K31/00

9. 发明公开

EP1796634A2 DELIVERING IRON TO AN ANIMAL 审中-公开
标题翻译：铁施用给动物
公开(公告)号：EP1796634A2
公开(公告)日：2007-06-20
申请号：EP05796901.6
申请日：2005-09-13
申请人： GILEAD SCIENCES, INC.
发明人： HU, Ning , JENSEN, Gerard M. , SKENES, Craig , YANG, Stephanie
IPC分类号： A61K9/10 , A61M36/14
CPC分类号： A61K33/26 , A61K9/0019 , A61K9/127 , A61K31/285
摘要： The invention provides a method for delivery iron to an animal. This invention further provides a method for treating iron deficiency in an animal.

10. 发明公开

EP1567130A2 METHOD OF DRUG LOADING IN LIPOSOMES BY GRADIENT 审中-公开
标题翻译：方法脂质体梯度药物CHARGE
公开(公告)号：EP1567130A2
公开(公告)日：2005-08-31
申请号：EP03790130.3
申请日：2003-11-26
申请人： GILEAD SCIENCES, INC.
发明人： HU, Ning , JENSEN, Gerard, M. , SULIVAN, Michele , YANG, Stephanie
IPC分类号： A61K9/127
CPC分类号： A61K9/127 , A61K9/1277 , A61K9/1278 , A61K31/137 , A61K31/55 , A61K31/704
摘要： A method for encapsulation of pharmaceutical agents (e.g., antineoplastic agents) in liposomes is provided, having preferably a high drug:lipid ratio. Liposomes can be made by a process that loads the drug by an active mechanism using a transmembrane pH gradient. Using this technique, trapping efficiencies approach 100%. Drug:lipid ratios employed are higher than for older traditional liposome preparations, and the release rate of the drug from the liposomes is reduced. After loading, residual acid is quenched with a quenching agent that is base permeable at low temperatures. The residual aciditiy is thus reduced and chemical stability (e.g. against hydrolysis) is enhanced. The stability of both the liposome and the pharmaceutical agent is thus maintained, prior to administration. The pH gradient is, however, present when the liposome is administered in vivo because the quenching agent rapidly exits the liposome.

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